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Items: 27

1.

Identification and biological evaluation of thiazole-based inverse agonists of RORγt.

Gege C, Cummings MD, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Nelen MI, Milligan C, Spurlino J, Xue X, Leonard K, Edwards JP, Fourie A, Goldberg SD, Hoffmann T.

Bioorg Med Chem Lett. 2018 May 15;28(9):1446-1455. doi: 10.1016/j.bmcl.2018.03.093. Epub 2018 Apr 3.

PMID:
29631962
2.

Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties.

Kinzel O, Steeneck C, Schlüter T, Schulz A, Gege C, Hahn U, Hambruch E, Hornberger M, Spalwisz A, Frick K, Perović-Ottstadt S, Deuschle U, Burnet M, Kremoser C.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3746-53. doi: 10.1016/j.bmcl.2016.05.070. Epub 2016 May 24.

PMID:
27268696
3.

Toxic cerebellar syndrome due to methotrexate.

Kinzel O, Verma RK, Wiest R, Mattle HP.

Pract Neurol. 2015 Jun;15(3):214-5. doi: 10.1136/practneurol-2014-001064. Epub 2015 Mar 26. No abstract available.

PMID:
25814514
4.

Knocking on FXR's door: the "hammerhead"-structure series of FXR agonists - amphiphilic isoxazoles with potent in vitro and in vivo activities.

Gege C, Kinzel O, Steeneck C, Schulz A, Kremoser C.

Curr Top Med Chem. 2014;14(19):2143-58. Review.

PMID:
25388536
5.

The nuclear bile acid receptor FXR controls the liver derived tumor suppressor histidine-rich glycoprotein.

Deuschle U, Birkel M, Hambruch E, Hornberger M, Kinzel O, Perović-Ottstadt S, Schulz A, Hahn U, Burnet M, Kremoser C.

Int J Cancer. 2015 Jun 1;136(11):2693-704. doi: 10.1002/ijc.29312. Epub 2014 Nov 13.

6.

FXR controls the tumor suppressor NDRG2 and FXR agonists reduce liver tumor growth and metastasis in an orthotopic mouse xenograft model.

Deuschle U, Schüler J, Schulz A, Schlüter T, Kinzel O, Abel U, Kremoser C.

PLoS One. 2012;7(10):e43044. doi: 10.1371/journal.pone.0043044. Epub 2012 Oct 9.

7.

Synthetic farnesoid X receptor agonists induce high-density lipoprotein-mediated transhepatic cholesterol efflux in mice and monkeys and prevent atherosclerosis in cholesteryl ester transfer protein transgenic low-density lipoprotein receptor (-/-) mice.

Hambruch E, Miyazaki-Anzai S, Hahn U, Matysik S, Boettcher A, Perović-Ottstadt S, Schlüter T, Kinzel O, Krol HD, Deuschle U, Burnet M, Levi M, Schmitz G, Miyazaki M, Kremoser C.

J Pharmacol Exp Ther. 2012 Dec;343(3):556-67. doi: 10.1124/jpet.112.196519. Epub 2012 Aug 23.

8.

Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 1.

Malancona S, Altamura S, Filocamo G, Kinzel O, Hernando JI, Rowley M, Scarpelli R, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4422-8. doi: 10.1016/j.bmcl.2011.06.024. Epub 2011 Jun 16.

PMID:
21737272
9.

Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2.

Kinzel O, Alfieri A, Altamura S, Brunetti M, Bufali S, Colaceci F, Ferrigno F, Filocamo G, Fonsi M, Gallinari P, Malancona S, Hernando JI, Monteagudo E, Orsale MV, Palumbi MC, Pucci V, Rowley M, Sasso R, Scarpelli R, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4429-35. doi: 10.1016/j.bmcl.2011.06.023. Epub 2011 Jun 16.

PMID:
21737263
10.

Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.

Abel U, Schlüter T, Schulz A, Hambruch E, Steeneck C, Hornberger M, Hoffmann T, Perović-Ottstadt S, Kinzel O, Burnet M, Deuschle U, Kremoser C.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4911-7. doi: 10.1016/j.bmcl.2010.06.084. Epub 2010 Jun 19.

PMID:
20638278
11.

Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).

Pescatore G, Branca D, Fiore F, Kinzel O, Bufi LL, Muraglia E, Orvieto F, Rowley M, Toniatti C, Torrisi C, Jones P.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1094-9. doi: 10.1016/j.bmcl.2009.12.026. Epub 2009 Dec 6.

PMID:
20031401
12.

Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.

Ferrigno F, Branca D, Kinzel O, Lillini S, Llauger Bufi L, Monteagudo E, Muraglia E, Rowley M, Schultz-Fademrecht C, Toniatti C, Torrisi C, Jones P.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1100-5. doi: 10.1016/j.bmcl.2009.11.087. Epub 2009 Nov 22.

PMID:
20022747
13.

Metabolism-related liabilities of a potent histone deacetylase (HDAC) inhibitor and relevance of the route of administration on its metabolic fate.

Fonsi M, Fiore F, Jones P, Kinzel O, Laufer R, Rowley M, Monteagudo E.

Xenobiotica. 2009 Oct;39(10):722-37. doi: 10.1080/00498250903082279.

PMID:
19569735
14.

Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.

Dessole G, Branca D, Ferrigno F, Kinzel O, Muraglia E, Palumbi MC, Rowley M, Serafini S, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4191-5. doi: 10.1016/j.bmcl.2009.05.112. Epub 2009 Jun 2.

PMID:
19540115
15.

Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.

Kinzel O, Llauger-Bufi L, Pescatore G, Rowley M, Schultz-Fademrecht C, Monteagudo E, Fonsi M, Gonzalez Paz O, Fiore F, Steinkühler C, Jones P.

J Med Chem. 2009 Jun 11;52(11):3453-6. doi: 10.1021/jm9004303.

PMID:
19441846
16.

3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates--a new class of HIV-1 integrase inhibitors.

Donghi M, Kinzel OD, Summa V.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):1930-4. doi: 10.1016/j.bmcl.2009.02.055. Epub 2009 Feb 20.

PMID:
19269170
17.

Optimization of a series of potent and selective ketone histone deacetylase inhibitors.

Pescatore G, Kinzel O, Attenni B, Cecchetti O, Fiore F, Fonsi M, Rowley M, Schultz-Fademrecht C, Serafini S, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5528-32. doi: 10.1016/j.bmcl.2008.09.003. Epub 2008 Sep 6.

PMID:
18809328
18.

Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.

Summa V, Petrocchi A, Bonelli F, Crescenzi B, Donghi M, Ferrara M, Fiore F, Gardelli C, Gonzalez Paz O, Hazuda DJ, Jones P, Kinzel O, Laufer R, Monteagudo E, Muraglia E, Nizi E, Orvieto F, Pace P, Pescatore G, Scarpelli R, Stillmock K, Witmer MV, Rowley M.

J Med Chem. 2008 Sep 25;51(18):5843-55. doi: 10.1021/jm800245z.

PMID:
18763751
19.

A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.

Jones P, Altamura S, De Francesco R, Paz OG, Kinzel O, Mesiti G, Monteagudo E, Pescatore G, Rowley M, Verdirame M, Steinkühler C.

J Med Chem. 2008 Apr 24;51(8):2350-3. doi: 10.1021/jm800079s. Epub 2008 Mar 28.

PMID:
18370373
20.

Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.

Muraglia E, Kinzel O, Gardelli C, Crescenzi B, Donghi M, Ferrara M, Nizi E, Orvieto F, Pescatore G, Laufer R, Gonzalez-Paz O, Di Marco A, Fiore F, Monteagudo E, Fonsi M, Felock PJ, Rowley M, Summa V.

J Med Chem. 2008 Feb 28;51(4):861-74. doi: 10.1021/jm701164t. Epub 2008 Jan 25.

PMID:
18217703
21.

A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies.

Kinzel O, Fattori D, Muraglia E, Gallinari P, Nardi MC, Paolini C, Roscilli G, Toniatti C, Gonzalez Paz O, Laufer R, Lahm A, Tramontano A, Cortese R, De Francesco R, Ciliberto G, Koch U.

J Med Chem. 2006 Sep 7;49(18):5404-7.

PMID:
16942012
22.

Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant.

Muraglia E, Kinzel OD, Laufer R, Miller MD, Moyer G, Munshi V, Orvieto F, Palumbi MC, Pescatore G, Rowley M, Williams PD, Summa V.

Bioorg Med Chem Lett. 2006 May 15;16(10):2748-52. Epub 2006 Feb 28.

PMID:
16503141
23.

A functionally orthogonal estrogen receptor-based transcription switch specifically induced by a nonsteroid synthetic ligand.

Gallinari P, Lahm A, Koch U, Paolini C, Nardi MC, Roscilli G, Kinzel O, Fattori D, Muraglia E, Toniatti C, Cortese R, De Francesco R, Ciliberto G.

Chem Biol. 2005 Aug;12(8):883-93.

24.
25.

A practical approach to the synthesis of hairpin polyamide-peptide conjugates through the use of a safety-catch linker.

Fattori D, Kinzel O, Ingallinella P, Bianchi E, Pessi A.

Bioorg Med Chem Lett. 2002 Apr 22;12(8):1143-7.

PMID:
11934575

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